January 27, 2023

Dutasteride is a 5-alpha reductase inhibitor that is indicated for treatment of BPH either alone or in combination. This drug inhibits conversion of testosterone to its more active form dihydrotestosterone (DHT). This results in reduced androgenic activities at prostate gland leading to decrease in its size.

Hi everyone today in this video let us discuss about the dutasteride what is this drag dutasteride is one of the drag which is used the treatment of benign prostatic hyperplasia which is commonly known as bph this is one of the disorder which results in the prostate enlargement under normal size of the prostate gland the urinary flow is normal through the urethra

But when this prostate gland is going to be enlarged it results in the constriction of the urethra which results in that decreased urinary flow so prostate enlargement may result in the decreased urinary flow as well as increased urinary frequency because the bladder is going to be filled with the urine but patients are unable to empty the bladder so decrease in

The urinary flow and increase the urinary frequency are the two important symptoms in the benign prostatic hyperplasia which resists in the incomplete emptying of the bladder in the patients so here the dutasteride can be used to treat the benign prostatic hyperplasia but how this drug acts this drug is going to inhibit the androgenic activities thereby can reduce

The prostate enlargement and improve the symptoms of the bph this deutocide can be given as monotherapy this drug can be used alone otherwise it can be used as a combination therapy so with which drug it is going to be combined in the benign prostatic hyperplasia we have seen that the prostate tissue is going to be enlarged so one of the drug is the dutasteride

Which is going to inhibit the androgenic activities thereby decrease the prostate growth but we can also use the other drugs which are going to relax the prostate tissue so here the dutasteride can be combined with the underdrag tamsulosin dutasted is a five alpha reductase inhibitor which inhibits the activation of the testosterone thereby inhibits the androgenic

Activities and tam solution is a alpha 1a blocker produce a relaxation of the prostate tissue in this way this combination can also be used to treat the benign prostatic hyperplasia but initially monotherapy is going to be suggested and when the monotherapy is unable to control the symptoms of the bph then combination therapy can be used so here the main action

Of the dutasteride is on the 5 alpha reductase inhibition so what is this 5 alpha reductase enzyme this enzyme is present as two isomeric forms it is present as a type 1 5 alpha reductase enzyme as well as type 2 5 alpha reductase enzyme this type 1 isoform is mainly present in the skin and liver which is response for the activation of the androgens at these

Organs and type 2 is mainly present on the reproductive tissue in the male genitalia this enzyme is response for the activation of the testosterone now on which enzyme this jutasteride is going to act now this drag is going to inhibit both type 1 as well as type 2 enzyme so it is nonselective for both isoforms thereby inhibits the androgenic activities at the

Reproductive tissue skin as well as liver on the other hand and the related drug is their finasteride which is only inhibiting the type 2 enzyme in this way 5 alpha reductase enzyme is very important for activation of the androgens but how this enzyme is going to produce the active metabolite of the androgens we know that the androgen in our physiological system

Is the testosterone you can see testosterone is a steroid nucleus with a delta four three one that means it is having a double bond at the fourth position and ketone at the third position now the double bond is at the fourth portion if it is saturated it results in the increased activity so now this testosterone can undergo the reduction by five alpha reductase

Enzyme thereby it can be converted into ender metabolite dihydrotestosterone which is commonly known as dht now you can see that at the fourth and fifth position there is a saturation so this is a simple reduction reaction where the testosterone is coming to dihydrotestosterone dht and this dht is more potent and the active form of the testosterone and this

Enzyme is going to be blocked by deutacerate thereby inhibits the activity of the testosterone in order to act on this enzyme duty cereal should also have some structural similarity now let’s see the structure of the dutasteride this is the structure of the dutasteride and you can observe again it is having a sterile nucleus but it is not having a double bond at

The fourth position instead it is having a nitrous at the fourth position so this drug is a four edge of steroid and it is having one double bond at the first and second portion and keto group at the third portion and even at the 17th position is having an amide which is attached with a phenyl ring with trifluoromethyl substitution so this is the dutasteride so

Jutasterad is having a similar sterile nucleus like the testosterone but it is having a nitrogen at the fourth position this structural similarity is responsible for the action of this drag on the 5 alpha reductase enzyme now let’s see how it acts we know that testosterone is one of the important androids in our physiological system this testosterone can enter

Into the cells where it is going to be converted into active form by the 5 alpha reductase enzyme so now this testosterone is going to be converted into its metabolite dht dihydrotestosterone this dihydrotestosterone can act on the androgen receptors which are present within the cytoplasm now once this dht is going to bind to these androgen receptors they will

Undergo the dimerization as well as autophosphorylation after this dimerization and autophosphorylation they can enter into the nucleus now these receptors are internalized into the nucleus where they are going to act on the dna to produce a gene transcription and this gene transcription is followed by protein synthesis in this way the dihydro testosterone can

Produce few of the proteins which produce the growth of the tissues and particularly these proteins can increase the growth of the prostate gland which resists in the enlargement of the prostate in this way androgens can increase the prostate enlargement which results in the decreased urinary flow and increased urinary frequency in the patients so in order to

Treat the bph the actions of the testosterone should be inhibited and here one of the important enzyme is the five alpha reductase enzyme so this is going to be inhibited by dutasteride so jutasteride is going to inhibit this five alpha reductase enzyme thereby it inhibits the androgenic actions on the prostate gland what are the side effects all side effects of

The dutasteride are related to the reproductive organs it can produce a breast enlargement and breast tenderness in the patients and you can also produce importance as well as ejaculation problems so failure of ejaculation can be observed without dutasteride and it can also produce a loss of liberal reduced sexual desire is observed with the tutasteride so all

These are the hormonal side effects produced by deutacide and apart from this it can also produce few other other side effects like the testicular pain dizziness and lightheadedness which are less absurd in the patients what are the contraindications the first contraindication is the pregnancy so this drug is categorized as a category x so this drug is strictly

Contraindicated in the pregnancy because the testosterone is going to be converted into dihydrotestosterone by the enzyme 5 alpha reductase enzyme this dihydrotestosterone dst is responsible for the development of the male genitalia so when the dutasteride is given it can inhibit the 5 alpha reductase enzyme thereby it inhibits the conversion of the testosterone

To the dht which results in the inhibition of the development of male genitalia in the male fetus that’s why in the pregnant woman this drug is strictly contraindicated similarly second one is a child bearing woman just like the previous one this duck can produce some risk to the male fetus so in the child bearing woman again this drug is counterindicated and

Deuterostatic can also be absorbed through the skin so that’s why the handling of this drug is also very important in the woman the woman should avoid the contact of the drug directly because the drug can be absorbed through the skin which can produce some abnormalities third one is a pediatric patients again in the pediatric patients this drug can reduce the

Growth of the genitalia and reproductive tissues so it should be contraindicated and fourth one is the patients with the hypersensitivity this drug can produce few of the hypersensitive reactions in few set of the inferior of the people so if any hypersensitive reactions are going to be developed this drug is contraindicated what are the drug interactions the

Calcium channel blockers like the varap mill and deltiasm they can reduce the clearance of the dutasteride therefore this drug should be carefully given with these calcium channel blockers similarly jutasteride is metabolized by cyp 3a4 enzymes so it can be converted into metabolites and strong cyp3f4 inputters like the retinoid can inhibit the metabolism of

The dutasteride thereby can increase the levels of this tag so enzyme inhibitor should be carefully given with the dutasteride how it is given this drug is given as a capsule at a dose of 0.5 mg and the dose of this drug again depends on how it is going to be prescribed if it is used for the monotherapy the dose is 0.5 mg once daily if it is given as a combination

Therapy with the alpha blockers then it can be given at a dose of again 0.5 mg dutasteride and 0.4 mg time cirocine again this combination given once daily in this way deutache diet is one of the drag which can be used as a monotherapy or combination therapy given at a dose of point family once daily and this like is particularly used to treat the benign prostatic

Hyperplasia where this drug inhibits the conversion of the testosterone into the dihydrotestosterone which is the active form of the androgens and by inhibition of this enzyme geotaste can inhibit the androgenic activities thereby it can reduce the enlargement of the prostate tissue in this way it can relieve the symptoms of the bph by reducing the androgenic

Activities so that’s about the jutasterite hope you have enjoyed this video if you like this video please subscribe to our channel share this video with your friends post your comments in the comment box thank you for watching this video

Transcribed from video
Dutasteride for Benign Prostatic Hyperplasia (BPH) By egpat